Heterocyclic sulphonylnitrometanes, process for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 207/48 (2006.01) A61K 31/33 (2006.01) C07D 209/08 (2006.01) C07D 209/44 (2006.01) C07D 211/96 (2006.01) C07D 215/58 (2006.01) C07D 217/22 (2006.01) C07D 265/30 (2006.01) C07D 277/04 (2006.01) C07D 277/16 (2006.01) C07D 295/26 (2006.01)

Patent

CA 2025664

(57)Abstract The invention concerns pharmaceutically useful heterocyclic nitromethane compounds of formula (1), in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula -NRa-, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R1, R2 and R3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R1, R2 and R3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completing ring Q is of 3 atoms then at least one of R1, R2 and R3 is hydrogen; and salts thereof. Other aspects of the invention include the production of the novel compounds by analogy processes and pharmaceutical compositions of the novel compounds and of (N)-(nitromethyl- sulphonyl)morpholine for use in the treatment of diabetic complications.

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